DERIVATIVES OF DIOXANE-2-ALKYL CARBAMATES, PREPARATION METHOD THEREOF AND APPLICATION OF SAME IN THERAPEUTICS

摘要

1,3-Dioxanylalkylcarbamate derivatives (I) are new. 1,3-Dioxanylalkylcarbamate derivatives of formula (I) and their salts, hydrates and solvates are new. [Image] R 1phenyl or naphthyl optionally substituted with halo, OH, CN, NO 2, 1-3C alkyl. 1-3C alkoxy, CF 3, OCF 3, benzyloxy, 3-6C cycloalkoxy or (3-6C)cycloalkyl(1-3C)alkoxy; R 2CHR 3CONHR 4, CH 2CF 3, imidazol-2-ylmethyl, benzimidazol-2-ylmethyl, or phenyl optionally substituted with halo, CN, NO 2, 1-3C alkyl. 1-3C alkoxy, CF 3 or OCF 3; R 3H or Me; R 4H, 1-3C alkyl, 3-5C cycloalkyl or 4-pyridylmethyl; n : 1-3. Independent claims are also included for: (1) two processes for preparing compounds (I); (2) intermediates of formula (Ia) and (VI). [Image] R 5Me or Et. ACTIVITY : Analgesic; Antimigraine; Antiarthritic; Antiemetic; Neuroleptic; Neuroprotective; Antidepressant; Nootropic; Antiparkinsonian; Hypotensive; Antiarrhythmic; Cardiant; Anticonvulsant; Nephrotropic; Cytostatic; Immunosuppressive; Antipsoriatic; Antiallergic; Antiparasitic; Virucide; Anti-HIV; Antibacterial; Antiinflammatory; Osteopathic; Ophthalmological; Uropathic. MECHANISM OF ACTION : Fatty acid amino hydrolase (FAAH) inhibitor. The most active compounds (unspecified) have IC50 values of 0.005-1 mu M in the FAAH assay described in Life Sciences, 56, 1999 (1995).